Brigatinib CAS 1197953-54-0

Product Description:

Product Name: brigatinib CAS NO: 1197953-54-0

Synonyms:

AP-26113;

Ap26113, brigatinib;

AP 26113;

Chemical & Physical Properties:

Appearance: Light yellow solid powder

Assay :≥98.0%

Density: 1.3±0.1 g/cm3

Boiling Point: 781.8±70.0℃at 760 mmHg

Flash Point: 426.6±35.7℃

Refractive Index: 1.641

Storage Condition: Dry, dark and at 0 – 4℃ for short term (days to weeks) or -20℃ for long term (months to years).

Solubility: Soluble in DMSO (2 mg /mL) or ethanol (10mg/mL)

Brigatinib (previously known as AP26113) is an investigational small-molecule targeted cancer therapy being developed by ARIAD Pharmaceuticals, Inc. Brigatinib has exhibited activity as a potent dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR).

ARIAD has begun a Phase 1/2 clinical trial of brigatinib based on cancer patients’ molecular diagnoses in September 2011.

ALK was first identified as a chromosomal rearrangement in anaplastic large cell lymphoma (ALCL). Genetic studies indicate that abnormal expression of ALK is a key driver of certain types of non-small cell lung cancer (NSCLC) and neuroblastomas, as well as ALCL. Since ALK is generally not expressed in normal adult tissues, it represents a highly promising molecular target for cancer therapy.

Epidermal growth factor receptor (EGFR) is another validated target in NSCLC. Additionally, the T790M “gatekeeper” mutation is linked in approximately 50 percent of patients who grow resistant to first-generation EGFR inhibitors. While second-generation EGFR inhibitors are in development, clinical efficacy has been limited due to toxicity thought to be associated with inhibiting the native (endogenous or unmutated) EGFR. A therapy designed to target EGFR, the T790M mutation but avoiding inhibition of native EGFR is another promising molecular target for cancer therapy.

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